HIGHLIGHTS OF PRESCRIBING INFORMATION
These highlights do not include all the information needed to usePIQRAY safely and effectively. See full prescribing information forPIQRAY.
PIQRAY(alpelisib)tablets, for oral use
Initial U.S. Approval: 2019
INDICATIONS AND USAGE
PIQRAY is a kinase inhibitor indicated in combination with fulvestrant for thetreatment of postmenopausal women, and men, with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative,PIK3CA-mutated, advanced or metastatic breast cancer as detected by anFDA-approved test following progression on or after an endocrine-basedregimen. (1)
DOSAGE AND ADMINISTRATION
Recommended dose: 300 mg (two 150 mg tablets) taken orally once dailywith food. (2.2)
For adverse reactions, consider dose interruption, dose reduction, ordiscontinuation. (2.3)
DOSAGE FORMS AND STRENGTHS
Tablets: 50 mg, 150 mg, 200 mg (3)
CONTRAINDICATIONS
Severe hypersensitivity to PIQRAY or to any of its components (4).
WARNINGS AND PRECAUTIONS
Severe Hypersensitivity: Permanently discontinue PIQRAY. Promptlyinitiate appropriate treatment. (5.1)
Severe Cutaneous Reactions: Cases of severe cutaneous reactions,including Stevens-Johnson syndrome (SJS) and Erythema Multiforme(EM) were reported. Do not initiate treatment in patients with a history ofSJS, EM, or Toxic Epidermal Necrolysis (TEN). Interrupt PIQRAY if signsor symptoms of severe cutaneous reactions are present, until etiology of thereaction has been determined. Consider consultation with a dermatologist.
Permanently discontinue PIQRAY if SJS, EM, or TEN is confirmed. (5.2)
Hyperglycemia: Severe hyperglycemia, including ketoacidosis, wasreported. The safety of PIQRAY in patients with Type 1 or uncontrolled Type 2 diabetes has not been established. Before initiating treatment withPIQRAY, test fasting plasma glucose (FPG), HbA1c, and optimize bloodglucose. After initiating treatment, monitor periodically. Initiate oroptimize anti-hyperglycemic medications as clinically indicated. Interrupt,reduce dose, or discontinue PIQRAY if severe hyperglycemia occurs. (2.3,5.3)
Pneumonitis: Severe cases of pneumonitis and interstitial lung disease havebeen reported. Monitor for clinical symptoms or radiological changes.
Interrupt or discontinue PIQRAY if severe pneumonitis occurs. (2.3, 5.4)
Diarrhea: Severe cases of diarrhea, including dehydration and acute kidneyinjury, have been reported. Most patients experience diarrhea (Grade ≤ 2)during treatment with PIQRAY. Advise patients to start antidiarrhealtreatment, increase oral fluids, and notify their healthcare provider ifdiarrhea occurs. Interrupt, reduce dose, or discontinue PIQRAY if severediarrhea occurs. (2.3, 5.5)
Embryo-Fetal Toxicity: PIQRAY can cause fetal harm. Advise patients ofpotential risk to a fetus and to use effective contraception (5.6, 8.1, 8.3).
Also, refer to the Full Prescribing Information of fulvestrant for pregnancyand contraception information.
ADVERSE REACTIONS
Most common adverse reactions including laboratory abnormalities (allgrades, incidence ≥ 20%) were glucose increased, creatinine increased,diarrhea, rash, lymphocyte count decreased, GGT increased, nausea, ALTincreased, fatigue, hemoglobin decreased, lipase increased, decreased appetite,stomatitis, vomiting, weight decreased, calcium decreased, gluc